5341-07-1Relevant academic research and scientific papers
Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms
Mehndiratta, Samir,Chen, Mei-Chuan,Chao, Yuh-Hsuan,Lee, Cheng-Hsin,Liou, Jing-Ping,Lai, Mei-Jung,Lee, Hsueh-Yun
, p. 74 - 84 (2020/11/10)
A series of 3-subsituted quinolinehydroxamic acids has been synthesised and evaluated for their effect on human lung cancer cell line (A549), human colorectal cancer cell line (HCT116) and HDAC isoforms 1, 2, 6, and 8. The results indicated that substitut
PHENANTHROLINE PHOSPHONIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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Paragraph 0090-0092, (2017/02/28)
The present invention relates to a novel phenanthroline phosphonic acid compound and a pharmaceutical salt thereof, as well as an application of the compound and the pharmaceutical salt thereof as collagen prolyl hydroxylase inhibitors in the preparation of drugs for preventing or treating collagen prolyl-4-hydroxylase related disease.
QUINOLINE DERIVATIVES FOR DIAGNOSIS AND TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 11; 12, (2016/11/28)
A new class of quinoline compounds is useful for the detection and treatment of Alzheimer's disease and other neurodegenerative diseases such as amyloidoses and tauopathies. The compounds can be synthesized in radiolabeled form for use as imaging agents,
5-Position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives
Kuninobu, Yoichiro,Nishi, Mitsumi,Kanai, Motomu
supporting information, p. 8092 - 8100 (2016/09/09)
We developed a copper-catalyzed 5-position-selective C-H trifluoromethylation of 8-aminoquinoline derivatives. The reaction proceeded with high functional group tolerance under mild conditions. In the case of quinolines with an amide, carbamate, urea, or sulfonamide group at the 8-position of quinoline moieties, a radical scavenger experiment indicated that the reaction proceeded via a radical pathway. The protecting group of an 8-amidoquinoline derivative could be removed by hydrolysis. On the other hand, the trifluoromethylation of 8-aminoquinolines was also promoted by other Lewis acids as well as a copper catalyst and proceeded even in the presence of a radical scavenger. These results indicated that the trifluoromethylation of 8-aminoquinolines proceeded via a Friedel-Crafts-type reaction. Interestingly, the copper salt works as either a catalyst for the formation of a CF3 radical or a Lewis acid to promote a Friedel-Crafts-type reaction, depending on the substrate.
Synthesis and structure activity relationship of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives as 5-HT6 receptor antagonists
Nirogi, Ramakrishna V.S.,Badange, Rajeshkumar,Gudla, Parandhama,Khagga, Mukkanti
, p. 3779 - 3784 (2014/08/05)
As part of our efforts to develop better therapies for the treatment of cognitive impairment associated with Alzheimer's disease and Schizophrenia, we have focused our research towards 5-HT6 receptor (5-HT6R) in order to identify potent and selective ligands for this purpose. Herein, we report the synthesis, structure activity relationship and biological evaluation of a novel series of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives, as 5-HT6 receptor (5-HT6R) antagonists. In this work, we have shown that moving from aryl sulfonamide platform to biaryl sulfone platform retains the 5-HT6.R affinity when tested in vitro in cell based reporter gene functional assay.
COMPOSITIONS AND METHODS FOR JAMM PROTEIN INHIBITION
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Page/Page column 107, (2014/05/24)
Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed.
Protonmotive force: Development of electrostatic drivers for synthetic molecular motors
Crowley, James D.,Steele, Ian M.,Bosnich, Brice
, p. 8935 - 8951 (2007/10/03)
Ferrocene has been investigated as a platform for developing protonmotive electrostatic drivers for molecular motors. When two 3-pyridine groups are substituted to the (rapidly rotating) cyclopentadienyl (Cp) rings of ferrocene, one on each Cp, it is shown that the (Cp) eclipsed, π-stacked rotameric conformation is preferred both in solution and in the solid state. Upon quaternization of both of the pyridines substituents, either by protonation or by alkylation, it is shown that the preferred rotameric conformation is one where the pyridinium groups are rotated away from the fully π-stacked conformation. Electrostatic calculations indicate that the rotation is caused by the electrostatic repulsion between the charges. Consistently, when the π-stacking energy is increased π-stacked population increases, and conversely when the electrostatic repulsion is increased π-stacked population is decreased. This work serves to provide an approximate estimate of the amount of torque that the electrostatically driven ferrocene platform can generate when incorporated into a molecular motor. The overall conclusion is that the electrostatic interaction energy between dicationic ferrocene dipyridyl systems is similar to the π-stacking interaction energy and, consequently, at least tricationic systems are required to fully uncouple the π-stacked pyridine substituents.
NITROGEN-CONTAINING HETEROARYL COMPOUNDS HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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Page 114; 115, (2008/06/13)
A compound of the formula (I): wherein Z4, Z5 and Z9 each is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; RA is a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.
4-Heteroparyl-1,4-diazabicyclo[3.2.2]nonane, preparation and therapeutic use thereof
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, (2008/06/13)
Compounds of the general formula (I) in which R1, R2, R3 and R4 each represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, cyano, hydroxyl, alkyl or alkoxy group, X represents either a nitrogen atom, in which case Z represents a group of the formula C—R5 or a nitrogen atom, or a group of the formula C—R6, in which case Z represents a nitrogen atom, R5 and R6 each represent a hydrogen or halogen atom or a trifluoromethyl, cyano, hydroxyl, (C1-C6)alkyl or (C1-C6)alkoxy group, and R7 represents a hydrogen atom or a (C1-C6)alkyl group. Use in therapy.
Polymer-supported phosphoramidites: Highly efficient and recyclable catalysts for asymmetric hydrogenation of dimethylitaconate and dehydroamino acids and esters
Doherty, Simon,Robins, Edward G.,Pal, Ibolya,Newman, Colin R.,Hardacre, Christopher,Rooney, David,Mooney, Damian A.
, p. 1517 - 1527 (2007/10/03)
Several novel phosphoramidites have been prepared by reaction of the primary amines para-vinylaniline, ortho-anisidine, 2-methoxyphenyl(4-vinylbenzyl)amine, 8-aminoquinoline and 3-vinyl-8-aminoquinoline with (S)-1,1′-bi-2-naphthylchlorophosphite, in the presence of base. Rhodium(I) complexes of these phosphoramidites catalyse the asymmetric hydrogenation of dimethylitaconate and dehydroamino acids and esters giving ee values up to 95%. Soluble non-cross linked polymers of the para-vinylaniline and 3-vinyl-8-aminoquinoline-based phosphoramidites have been prepared by free radical co-polymerisation with styrene in the presence of AIBN as initiator. The corresponding [Rh(COD)]+ complexes serve as recyclable catalysts for the asymmetric hydrogenation dimethylitaconate and dehydroamino acids and esters to give ee values up to 80%.
